CID 16020046

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Chemical Structure| 834903-43-4 同义名 : C390-0219
CAS号 : 834903-43-4
货号 : A843612
分子式 : C25H19N3O4
纯度 : 99%+
分子量 : 425.436
MDL号 : MFCD06196075
存储条件：

Pure form Sealed in dry,2-8°C

In solvent -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 105 mg/mL(246.81 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
描述 The G protein-coupled receptor 55 (GPR55), a lysophosphatidylinositol (LPI) receptor that is responsive to certain cannabinoids, has been implicated in several (patho)physiologic functions. CID-16020046 (40 nM – 10 μM) acts as an inverse agonist, inhibiting GPR55 constitutive activity with an IC50 of 0.15 μM. In HEK-GPR55 cells, pretreatment with increasing concentrations of CID-16020046 inhibited GPR55 agonist-induced intracellular Ca2+ release. Further, 2.5 μM CID-16020046 significantly inhibited the LPI (a GPR55 agonist)-induced ERK1/2 phosphorylation, GPR55 internalization and GPR55-mediated transcription factor activation in HEK-GPR55 cells[3]. In the DSS (dextran sulfate sodium) and TNBS (trinitrobenzene sulfonic acid) colitis models, treatment with CID-16020046 at a dosage of 20 mg/kg significantly reduced macroscopic scores and MPO (myeloperoxidase) activity as compared to vehicle-treated animals[4].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.35mL

0.47mL

0.24mL

11.75mL

2.35mL

1.18mL

23.51mL

4.70mL

2.35mL
参考文献

[1]AlSuleimani YM, Hiley CR. The GPR55 agonist lysophosphatidylinositol relaxes rat mesenteric resistance artery and induces Ca(2+) release in rat mesenteric artery endothelial cells. Br J Pharmacol. 2015 Jun;172(12):3043-57.

[2]Kargl J, Brown AJ, et al. A selective antagonist reveals a potential role of G protein-coupled receptor 55 in platelet and endothelial cell function. J Pharmacol Exp Ther. 2013 Jul;346(1):54-66.

[3]Kargl J, Brown AJ, Andersen L, Dorn G, Schicho R, Waldhoer M, Heinemann A. A selective antagonist reveals a potential role of G protein-coupled receptor 55 in platelet and endothelial cell function. J Pharmacol Exp Ther. 2013 Jul;346(1):54-66

[4]Stančić A, Jandl K, Hasenöhrl C, Reichmann F, Marsche G, Schuligoi R, Heinemann A, Storr M, Schicho R. The GPR55 antagonist CID16020046 protects against intestinal inflammation. Neurogastroenterol Motil. 2015 Oct;27(10):1432-45